Biochem/physiol Actions

TH-257 is a potent, type III allosteric LIM-kinase (LIMK1 & LIMK2) inhibitor (LIMK1/2 IC50 in nM = 48/29 by cell-free kinase assay and 250/150 by live cell NanoBRET assay using respective transfectants) that targets LIMK1/2 DFG-out conformation in a non-ATP-competitive manner and exhibits no significant off-target activity by KINOMEscan assay at 1 µM. TH-263 is a structure analog and the recommended negative control for TH-257. For characterization details of TH-257, please visit the TH-257 probe summary on the Structural Genomics Consortium (SGC) website.TH-263 is the negative control for the active probe, TH-257. TH-263 is available from Sigma. To learn more about and purchase TH-263, click here.To learn about other SGC chemical probes, visit sigma.com/sgc

Features and Benefits

TH-257 is a chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.